Crofelemer is a botanical-derived pharmaceutical active ingredient with antisecretory and antidiarrheal activity. It is a purified oligomeric proanthocyanidin derived from the latex of Croton lechleri, a plant traditionally used in South American medicine.
Crofelemer is a complex botanical oligomer rather than a conventional single small-molecule API. It consists primarily of oligomeric proanthocyanidin structures and acts locally within the gastrointestinal tract.
Crofelemer is identified by CAS No. 91771-32-3 and is the active pharmaceutical ingredient in the approved product Mytesi.
Crofelemer acts locally in the intestinal lumen and inhibits two major chloride ion channels, CFTR (cystic fibrosis transmembrane conductance regulator) and CaCC (calcium-activated chloride channels). By reducing chloride secretion into the intestinal lumen, crofelemer decreases associated water secretion and helps reduce stool fluidity.
Crofelemer is indicated for the symptomatic relief of noninfectious diarrhea in adults with HIV/AIDS receiving antiretroviral therapy. It is administered orally as delayed-release tablets.
Crofelemer can be supplied for applicable pharmaceutical development, formulation and manufacturing requirements, subject to botanical raw-material controls, quality requirements and applicable regulatory standards.
Because crofelemer is a botanical complex substance, quality control may include identity, oligomeric profile, total proanthocyanidin content, chromatographic fingerprint, related substances, residual solvents, elemental impurities, microbial quality and other applicable critical quality attributes.
Final acceptance criteria should always be based on the approved product specification, validated analytical methods and batch-specific Certificate of Analysis (CoA).
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 0.5% |
| Melting Point | 150°C – 154°C |